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| Type |
Poster Presentation |
| Area |
Organic Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
ORGN.P-169 |
| Subject |
Bioactive Homoisoflavonoids: Synthesis and Antiinflammatory Activity
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| Authors |
Damodar Kongara, Jong-Gab Jun*, Jeong Tae Lee*
Department of Chemistry and Institute of Applied Chemistry, Hallym University, Korea, Hallym University, Korea
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| Abstract |
This study describes the first synthesis of natural homoisoflavonoids, (±)-portulacanones A-C (4, 8 and 9), portulacanone D (6) isolated from Portulaca oleracea L (POL) and their derivatives (3, 5 and 7) along with the synthesis of known derivatives (1 and 2) and also evaluation of their in vitro inhibitory effect against nitric oxide (NO) production in LPS-induced RAW-264.7 macrophages. All the compounds exhibited a concentration-dependent inhibitory effect and had no significant cytotoxicity to the macrophages at their effective concentration for the inhibition of NO production. Among them, compounds 3 (97.2% at 10 μM;IC50 = 1.26 µM) followed by 6 (92.5% at 10 μM; IC50 = 2.09 µM), 1 (91.4% at 10 μM; IC50 = 1.75 µM) and 7 (83.0% at 10 μM; IC50 = 2.91 µM) exhibited pronounced inhibition from the series. The obtained results were further correlated with the suppressed expression of iNOS induced by LPS. On the whole, compound 3 is expected to serve as a lead structure that merits further investigation for a NO production-targeted anti-inflammatory drug development and also could evidence the practicality of POL as a folklore medicinal plant in the treatment of inflammatory diseases where NO is involved. |
| E-mail |
kongaradamu@gmail.com |
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123rd General Meeting of the KCS